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Method for refining telmisartan

A technology for telmisartan and a purification method, applied in the field of chemistry, can solve the problems of cumbersome process, long process route and the like, and achieve the effects of simple process route, good product quality and good product color

Inactive Publication Date: 2012-07-18
JIANGXI SYNERGY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this method has a long process route and a cumbersome process

Method used

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  • Method for refining telmisartan
  • Method for refining telmisartan
  • Method for refining telmisartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1) prepare the crude product of telmisartan potassium salt

[0035] Put 500ml of isopropanol, 65g of telmisartan (0.126mol, content 98%), and 8.0g of potassium hydroxide (0.143mol) into a 1000ml four-necked bottle and stir, heat up to 75-80°C to dissolve, add 6.5g of activated carbon, And decolorize at this temperature for 1 hour, filter, the filtrate is cooled to 0° C. to crystallize for 8 hours, filter, and dry the filter cake under reduced pressure at 60° C. for 8 hours to obtain 62 g of crude telmisartan potassium salt.

[0036] 2) Refined Telmisartan Potassium Salt

[0037] Put 240ml of isopropanol into a 500ml four-necked bottle, 120% of ethyl acetate, 62g of crude telmisartan potassium salt, dissolve at 75-80°C, add 5g of activated carbon to decolorize for 1 hour, filter, and cool the filtrate to 0°C to crystallize for 8 hours. After filtering, the filter cake was dried under reduced pressure at 60° C. for 8 hours to obtain 58 g of refined telmisartan potassium ...

Embodiment 2

[0041] 1) prepare the crude product of telmisartan potassium salt

[0042] Put 500ml of isopropanol, 65g of telmisartan (0.126mol, content 98%), and 8.0g of potassium hydroxide (0.143mol) into a 1000ml four-necked bottle and stir, heat up to 75-80°C to dissolve, add 6.5g of activated carbon, And decolorize at this temperature for 1 hour, filter, the filtrate is cooled to 0° C. to crystallize for 8 hours, filter, and the filter cake is dried under reduced pressure at 60° C. for 8 hours to obtain 66 g of crude telmisartan potassium salt.

[0043] 2) Refined Telmisartan Potassium Salt

[0044] Put 350ml of isopropanol and 66g of crude telmisartan potassium salt into a 500ml four-necked bottle, heat up to 75-80°C to dissolve, add 5g of activated carbon to decolorize for 1 hour, filter, cool the filtrate to 0°C to crystallize for 8 hours, filter, filter cake Dry under reduced pressure at 60°C for 8 hours to obtain 62g of refined telmisartan potassium salt

[0045] 3) hydrolysis o...

Embodiment 3

[0048] 1) prepare the crude product of telmisartan potassium salt

[0049] Into the 1000ml four-necked bottle, 500ml of isopropanol, 65g of telmisartan (0.126mol, content 98%), and 60ml of 23.7% potassium carbonate water solution (0.143mol) were successively put into the bottle and stirred, heated to 75-80°C to dissolve, and added 6.5 g activated carbon, and decolorized at this temperature for 1 hour, filtered, and the filtrate was cooled to 0° C. to crystallize for 8 hours, filtered, and the filter cake was dried under reduced pressure at 60° C. for 8 hours to obtain 56 g of crude product of telmisartan potassium salt.

[0050] 2) Refined Telmisartan Potassium Salt

[0051] Put 350ml of isopropanol and 56g of crude telmisartan potassium salt into a 500ml four-necked bottle, dissolve at 75-80°C, add 5g of activated carbon to decolorize for 1 hour, filter, cool the filtrate to 0°C to crystallize for 8 hours, filter, filter cake Dry under reduced pressure at 60°C for 8 hours to...

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Abstract

The invention discloses a method for refining telmisartan, which comprises the following process routes of: I, reacting a coarse telmisartan product with alkali in water, an organic solvent or a mixed solvent A consisting of organic solvent and water to obtain a coarse product of telmisartan salt; II, re-crystallizing the coarse product of the telmisartan salt in an organic solvent or a mixed solvent B consisting of organic solvent and water to obtain refined telmisartan salt; and III, hydrolyzing and crystallizing the obtained refined telmisartan salt to obtain colorless to white refined telmisartan crystal. In order to reduce colored impurities in the refined telmisartan and improve the purity of a product at the same time, an active carbon decolorizing operation can be increased in thesteps I to III of the refining method. The method has simple process routes, and does not need to use a solvent with high boiling point in each step; and the finished product has no problem of solvent residue, the product has good quality, and the purity can reach over 99.8 percent.

Description

technical field [0001] The invention belongs to the field of chemistry, in particular to a method for refining telmisartan. Background technique [0002] Telmisartan, the chemical name is 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl Base-2-carboxylic acid (CAS accession number is 144701-48-4), molecular formula is C 33 h 30 N 4 o 2 , the molecular weight is 514.63, and the molecular structure is shown in 1; the pure product is a colorless to white crystal with a melting point of 261-263°C. Telmisartan, as an angiotensin (AT) II receptor antagonist, is a new type of antihypertensive drug. The compound was developed by Boehringer Ingethiem in Germany, and it was first launched in the United States in March 1999, and in Germany in the same year. [0003] [0004] In industrial preparations, telmisartan crystals are usually used as raw materials to prepare clinical preparations. The synthesized crude telmisartan contains more im...

Claims

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Application Information

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IPC IPC(8): C07D235/18
Inventor 蒋元森徐烘材彭建武赵伟蒋纬纲
Owner JIANGXI SYNERGY PHARMA
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